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I3 Exam 3 > Malaria Drugs (Ceryak) > Flashcards

Malaria Drugs (Ceryak) Flashcards

1
Q

Name artemisinins (2)

A
  • artemether

- artesunate

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2
Q

Quinolines (3)

A
  • chloroquine phosphate
  • quinine sulfate/quinidine gluconate
  • primaquine
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3
Q

Adjunctive with quinolines (2)

A
  • doxycycline

- clindamycin

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4
Q

Artemisinins target species

A

P. falciparum and P. vivax

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5
Q

How do artemisinins function as anti-malaria

A

endoperoxide moeity (free radial production)

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6
Q

Artemisinins resistance due to

A

counterfeit drugs

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7
Q

Which artemisinin is given orally and which is IV/rectal?

A

Oral: artemether

IV/Rectal” artesunate

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8
Q

How are artemisinins absorbed, metabolized, and excreted

A

Rapid absorptions, metabolism (CYP), biliary excretion

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9
Q

Describe the artemisinin half life; prophylaxis?

A

Short! (1-2 hours); not useful for prophylaxis; not good as monotherapy

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10
Q

Artemisinin-based combo therapues (ACTs)

A

increase efficacy and decrease resistance

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11
Q

Artemisinin adverse effects

A
  • generally well-tolerated, not recommended for children <5kg or during 1st trimester of pregnancy
  • reduced RBC and neutrophils; transient heart block (rare, dose-related, reversible)
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12
Q

Coartem =

A

artemether and lumefantrine; which both target blood stages

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13
Q

What is beneficial about coartem?

A

large Vd and 4-5 day half-life

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14
Q

Coartem problem

A

substantial drug-drug interaction with antiretrovirals/protease inhibitors (may need to increase dose)

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15
Q

How should pts take ACTs?

A

with fatty food or whole milk (if pt vomits within 30 min, repeat dose)

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16
Q

What pts are ACTs contraindicated in?

A

Cardiac arrhythmias, cardiac disease

17
Q

How do you get artesunate?

A

CDC!

18
Q

Quinolines and related compounds mechansim

A

interfere with heme digestion

19
Q

Chloroquine mechanism of action

A
  • plasmodium digest host cell hemoglobin
  • process releases large amts of heme, which is toxic to plasmodium
  • normally, plasmodium polymerizes heme to nontoxic hemozoin
  • chloroquine prevents polymerization to hemozoin
20
Q

Chloroquine resistance

A

pfcrt mutation - increased drug efflux

21
Q

Is chloroquine safe in pregnancy?

A

Yes!

22
Q

Oral chloroquine adverse effects

A
  • Visual disturbances
  • pruritis in African descent
  • rare hemolysis w/ pt w/ G6PD deficiency
  • discoloration of nail beds/mucous membranes
23
Q

Chloroquine parental doses > 5g

A

usually fatal!

-CV and CNS (irreversible retinopathy, arrhythmias, etc.)

24
Q

What pt is chloroquine contraindicated in?

A
  • pt w/ epilepsy/myasthenia gravis bc affects neuro-muscular transmission
  • pt w/ psoriasis/porphyria cutanea tarda
25
Q

Chloroquine caution in pt w/…

A
  • pt w/ advanced liver or GI disease, neurological or blood disorders (G6PD deficiency)
  • pt w/ cardiac dysarhythmias
26
Q

What to avoid while taking chloroquine

A
  • kaolin (clay mineral) and Ca2+/Mg2+ containing antacids (delay GI absorption)
  • concomitant administration of cimetidine (inhibits metabolism of chloroquine)
27
Q

Quinine use against…

A

chloroquine-R and MDR P. falciparum asexual blood stages, gametocyticidal against P. vivax and P.ovale

28
Q

Quinine mechanism

A

interferes w/ heme digestion

29
Q

What is different about IV quinine?

A

more potent/toxic

30
Q

Quinine absorption, metabolism, excretion

A

Readily absorbed (good tissue distribution in CNS and placenta); hepatic metabolism CYP3A4; renal excretion

31
Q

Quinine resistance

A

Pfmdr1 gene amplification (pumps out drug)

32
Q

Quinine adverse effects (dose-related toxicities)

A

-cinchonism = tinnitus, deafness, visual disturbance, headache, nausea, vomiting, dizziness, postural hypotension (reversible)

33
Q

Quinine adverse effects (hypersensitivity)

A

rash, urticaria, angioedema, bronchospams

-blackwater fever: severe hemolysis; hemoglobinemia

34
Q

When do you stop quinine treatment?

A

Hemoglobinuria

35
Q

Increased hemolysis with quinines in pt w/…

A

G6PD deficiency

36
Q

Quinine contraindicated in pt w/…

A

pt w/ tinnitus/optic neurititis

37
Q

Quinine caution in pt w/…

A
  • pt w/ hypersensitivity (discontinue if evidence of hemolysis)
  • pt w/ cardiac dysrhythmias
  • pregnancy (possibly safe)
  • decrease dose w/ renal insufficiency
  • aluminum/magnesium-containing antacids delay GI absorption
  • CYP3A4 inhibition

I3 Exam 3 (9 decks)

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